Betulin is used as a raw material for organic synthesis of betulinic acid, betulonic acid or derivatives thereof.

It was scientifically discovered in the paper [Pisha, E. et al., (1995) J. M. nature Medicine, 1, 1046-1051] that betulinic acid has antitumor activity in melanomas (for example, MEL-2, MEL-2 and MEL-4).
Further, it was published in the paper [Fujioka, T. et al. (1994) J. Nat. Prod. 57, 243-247] that betulinic acid has anti-HIV activity in H9 lymphocytic cells.
Further, it was published in the paper [Yunhao Gong et al. Antiviral Research 64 (2004) 127-130] that betulin exhibits antiviral effects upon herpes simplex viruses when it is mixed with acyclovir.
Further, it was disclosed in PCT/US2005/039068 (WO2006/050158 A2) by GLINSKI that betulin ether derivatives were applied to functional cosmetics in order to obtain the effects of skin and hair protection in skin moisturizers, antiperspirants, anti-wrinkle treatment creams, hair depilatories and the like.
Moreover, the present inventors, P. Allaway et al., have recently insisted through U.S. Pat. No. 7,365,221B2 that monoacylated betulin and dihydrobetulin derivatives have potent anti-HIV activity.
Betuloinic acid is represented by the following Chemical Formula:

Betulonic acid is synthesized by Jones oxidation of betulin extracted from the bark of a birch using an organic solvent. Betulonic acid is not easily dissolved in a biocompatible solvent, but has useful biological characteristics such as anti-cancer activity, anti-inflammatory activity, etc.
Referring to related prior arts, it was disclosed in WO 2007/141398 A1 that derivatives of 28-eugenol ester betulonic acid, 28-aspartateamide dimethyl ester betulonic acid, 28-acetate betulonic acid and the like exhibit anti-microbial effects.
Further, it was disclosed in the papers [Kobayashi et al., J. Org. Chem. 66:6626-6623(2001)] and [Zhao et al., J. Org. Chem. 69:270-279(2004)] and Patent document [Saxena et al., US2006/0154903 A1] that betulonic acid amide derivatives are prepared by synthesis of betulonic acid and lysine. Here, these betulonic acid amide derivatives have attracted considerable attention since they were verified to have an effect of suppressing the growth of prostatic cancer cells (LNCaP, PC-3, DU-145). Boc-Lysinated betulonic acid monomer ester (referred to as Boc-Lys-BOA monomer ester) is obtained by organic synthesis of betulonic acid and Boc-Lys(Cbz)-OH, and Boc-Lysinated betulonic acid (referred to as Boc-Lys-BOA), which is known to have an effect on prostatic cancer cells in-vivo and in-vitro experiments thereof, is hydrolysis of betulonic acid and Boc-Lys(Cbz)-OH.
In order to use the above-mentioned derivatives and synthetic materials as medical drugs suitable for a human body, high-purity Boc-lysinated betulonic acid monomer ester and high-purity Boc-lysinated betulonic acid having a purity of 99% or more must be obtained by an advanced purification method for removing polar and nonpolar substances during a synthesis process. However, such an advanced purification method has not been proposed yet.